Unprecedented and Biomimetic approach to Drug Discovery

Researchers have developed a new class of small molecules with the help of a novel approach that can help in accelerating the process of drug discovery.

This research has been done by the scientists on the Florida campus of The Scripps Research Institute led by Scripps Research Associate Professor Glenn Micalizio and published online in the November 20 issue of the journal Nature Chemistry.Chiral Oligomers of Pentanoic Amides, COPA

This novel approach of accelerating the drug discovery process has been developed on inspiration of natural process.

This approach has combined the power of synthetic chemistry with advanced screening technologies and could enhance the availability of possible synthetic compounds to be used as drugs. With this approach, substantial molecular limitations will be overcome and synthesis and screening of small molecules could be done with the same state-of-the-art approach.

Scientists have improved the process of high-throughput screening in the modern drug discovery process, in which a large number of molecules are evaluated for activity in the area of interest. Moleculesm, in that process, largely come from commercially available materials having structures unrelated to natural products.

Micalizio said,

This divergence in structure between natural products and commercially available synthetics lies at the heart of our inquiry. Why should we limit discovery of therapeutic leads to compound collections that are influenced by concerns relating to commercial availability and compatibility with an artificial set of constraints associated with the structure of modern screening centers?

They mimicked the process of “oligomerization” and joined it with the synthetic design to produce molecules. Oligomerization is the natural process of development of oligomers from monomers. Oligomers are the types of polymers with less than five monomer units.

With the same approach, researchers worked on 160,000-member compound collection and identify “non-covalent synthetic ligand to the DNA-binding domain of the p53 transcription factor”. p53 regulates a number of genes in cell cycle control and death.


Claudio Aquino, Mohosin Sarkar, Michael J. Chalmers, Kimberly Mendes, Thomas Kodadek & Glenn C. Micalizio, (2011). A biomimetic polyketide-inspired approach to small-molecule ligand discovery. Nature Chemistry, doi:10.1038/nchem.1200


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